Tolterodine Tartrate (124937-52-6)

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Product Detail

Mechanism:

Tolterodine is a competitive muscarinic receptor antagonist and acts as an antagonist of acetylcholine at postganglionic muscarinic receptors.. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. Tolterodine has been shown to inhibit carbachol-induced contraction of isolated bladder preparations from rats, guinea pigs, and man. It inhibits contractions of the detrusor muscle from the guinea pig, and electrically induced contractions of human detrusor muscle from stable and overactive bladders ex-vivo.
After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative (5-HMT), the major pharmacologically active metabolite. 5-HMT, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and 5-HMT exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels.
Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.

Storage conditions: Room temperature

Packaging: polyethylene nylon plastic bag

CAS Number: 124937-52-6

Formula: C26H37NO7

Molecular Weight: 475.6 g/mol

Method of Analysis: In house

Application:

Tolterodine is an antimuscarinic drug that is used for treatment of overactive bladder with symptoms of urinary frequency, urgency, and leakage.